UY34959A - DIHYDROPIRIDONE P1 AS INHIBITORS OF THE XIA FACTOR - Google Patents

DIHYDROPIRIDONE P1 AS INHIBITORS OF THE XIA FACTOR

Info

Publication number
UY34959A
UY34959A UY0001034959A UY34959A UY34959A UY 34959 A UY34959 A UY 34959A UY 0001034959 A UY0001034959 A UY 0001034959A UY 34959 A UY34959 A UY 34959A UY 34959 A UY34959 A UY 34959A
Authority
UY
Uruguay
Prior art keywords
inhibitors
compounds
dihydropiridone
present
xia factor
Prior art date
Application number
UY0001034959A
Other languages
Spanish (es)
Inventor
Yang Wu
James R Corte
Paul J Gilligan
Donald J P Pinto
William R Ewing
Wang Yufeng
Original Assignee
Bristol Myers Squibb Company Una Corporación Del Estado De Delaware
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Company Una Corporación Del Estado De Delaware filed Critical Bristol Myers Squibb Company Una Corporación Del Estado De Delaware
Publication of UY34959A publication Critical patent/UY34959A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

La presente invención provee compuestos de la Fórmula (VIII), o estereoisómeros, tautómeros o sales de aquellos aceptables desde el punto de vista farmacéutico, en donde todas las variables son como se definen en la presente. Estos compuestos son inhibidores selectivos del factor XIa o inhibidores duales de FXIa y calicreína plasmática. La presente invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos y a métodos para tratar trastornos tromboembólicos y/o inflamatorios mediante su uso.The present invention provides compounds of the Formula (VIII), or stereoisomers, tautomers or salts of those pharmaceutically acceptable, wherein all the variables are as defined herein. These compounds are selective inhibitors of factor XIa or dual inhibitors of FXIa and plasma kallikrein. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods for treating thromboembolic and / or inflammatory disorders by use.

UY0001034959A 2012-08-03 2013-08-02 DIHYDROPIRIDONE P1 AS INHIBITORS OF THE XIA FACTOR UY34959A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261679197P 2012-08-03 2012-08-03
US201361786992P 2013-03-15 2013-03-15

Publications (1)

Publication Number Publication Date
UY34959A true UY34959A (en) 2014-01-31

Family

ID=48949289

Family Applications (1)

Application Number Title Priority Date Filing Date
UY0001034959A UY34959A (en) 2012-08-03 2013-08-02 DIHYDROPIRIDONE P1 AS INHIBITORS OF THE XIA FACTOR

Country Status (26)

Country Link
US (2) US9376444B2 (en)
EP (1) EP2882734B1 (en)
JP (1) JP6082462B2 (en)
KR (1) KR20150038369A (en)
AR (1) AR093759A1 (en)
AU (1) AU2013296258A1 (en)
BR (1) BR112015002293A2 (en)
CA (1) CA2880898A1 (en)
CY (1) CY1118450T1 (en)
DK (1) DK2882734T3 (en)
EA (1) EA025392B1 (en)
ES (1) ES2605824T3 (en)
HR (1) HRP20161378T1 (en)
HU (1) HUE031582T2 (en)
IL (1) IL237012A0 (en)
LT (1) LT2882734T (en)
MX (1) MX361370B (en)
PL (1) PL2882734T3 (en)
PT (1) PT2882734T (en)
RS (1) RS55581B1 (en)
SG (1) SG11201500270RA (en)
SI (1) SI2882734T1 (en)
SM (1) SMT201700003B (en)
TW (1) TW201410666A (en)
UY (1) UY34959A (en)
WO (1) WO2014022766A1 (en)

Families Citing this family (26)

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TW201319068A (en) 2011-08-05 2013-05-16 必治妥美雅史谷比公司 Cyclic P1 linkers as factor XIa inhibitors
TW201311689A (en) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 Novel macrocycles as factor XIa inhibitors
ES2699226T3 (en) 2011-10-14 2019-02-08 Bristol Myers Squibb Co Substituted tetrahydroisoquinoline compounds as inhibitors of factor XIa
ES2579832T3 (en) 2011-10-14 2016-08-17 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
CA2851810C (en) 2011-10-14 2020-01-07 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
BR112015007937A2 (en) 2012-10-12 2017-07-04 Bristol Myers Squibb Co crystalline forms of a factor xia inhibitor
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US10081623B2 (en) 2014-09-04 2018-09-25 Bristol-Myers Squibb Company Diamide macrocycles that are FXIa inhibitors
NO2721243T3 (en) * 2014-10-01 2018-10-20
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
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WO2017019821A1 (en) 2015-07-29 2017-02-02 Bristol-Myers Squibb Company Factor xia new macrocycle bearing a non-aromatic p2' group
JP6629958B2 (en) 2015-07-29 2020-01-15 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Macrocyclic factor XIa inhibitors bearing alkyl or cycloalkyl P2 'groups
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EP3371162B1 (en) * 2015-10-29 2022-01-26 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
KR20180117156A (en) * 2016-03-02 2018-10-26 브리스톨-마이어스 스큅 컴퍼니 Diamide macrocycle with factor XIa inhibitory activity
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WO2021013209A1 (en) 2019-07-23 2021-01-28 南京明德新药研发有限公司 Macrocyclic derivatives as factor xia inhibitors

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ES2579832T3 (en) 2011-10-14 2016-08-17 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
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Also Published As

Publication number Publication date
IL237012A0 (en) 2015-03-31
CA2880898A1 (en) 2014-02-06
PL2882734T3 (en) 2017-05-31
US9376444B2 (en) 2016-06-28
ES2605824T3 (en) 2017-03-16
WO2014022766A1 (en) 2014-02-06
SG11201500270RA (en) 2015-03-30
CY1118450T1 (en) 2017-06-28
JP2015524443A (en) 2015-08-24
AR093759A1 (en) 2015-06-24
MX2015000919A (en) 2015-09-21
BR112015002293A2 (en) 2017-07-04
US20150166550A1 (en) 2015-06-18
AU2013296258A1 (en) 2015-03-19
TW201410666A (en) 2014-03-16
SI2882734T1 (en) 2017-01-31
PT2882734T (en) 2016-12-09
HRP20161378T1 (en) 2016-12-02
RS55581B1 (en) 2017-06-30
JP6082462B2 (en) 2017-02-15
CN104520289A (en) 2015-04-15
EP2882734B1 (en) 2016-10-12
HUE031582T2 (en) 2017-07-28
EP2882734A1 (en) 2015-06-17
DK2882734T3 (en) 2017-01-30
EA201590284A1 (en) 2015-05-29
SMT201700003B (en) 2017-03-08
LT2882734T (en) 2016-12-12
MX361370B (en) 2018-12-05
US20140038969A1 (en) 2014-02-06
EA025392B1 (en) 2016-12-30
KR20150038369A (en) 2015-04-08

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